Drug intelligence / Profile preview

dasatinib + quercetin

Development stage
Preclinical
Lead developer
Mayo Clinic investigators
Modality
Small Molecules
Administration
Oral
01

Overview

Dasatinib + quercetin is a senolytic drug combination consisting of the tyrosine kinase inhibitor dasatinib and the flavonoid antioxidant quercetin. This combination has been shown to selectively eliminate senescent cells, which accumulate with age and contribute to age-related tissue dysfunction, inflammation, and chronic diseases. In preclinical studies in aged mice, dasatinib plus quercetin reduced markers of cellular senescence (such as p16^Ink4a^ and p21^Cip1^) as well as inflammatory cytokines (including Cxcl1, Il1β, Il6, Mcp1, Tnfα) in multiple tissues including the intestine. The treatment also modulated gut microbiome composition. Dasatinib acts primarily by inhibiting multiple tyrosine kinases involved in cell survival pathways; quercetin is a plant-derived polyphenol that inhibits PI3K/AKT pathways among others. Together they act synergistically to induce apoptosis specifically in senescent cells[1][2].

Brand names
dasatinib + quercetin
Other names
D+Qdasatinib and quercetin combinationsenolytic combination of dasatinib and quercetin
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)BCL-2 (BCL-2 family)AKT (RAC-alpha serine/threonine-protein kinase)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)HIF1A (Hypoxia-inducible factor 1-alpha)SFK (SRC family kinases)EPHA2 (Ephrin type-A receptor 2)

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